σ2 受体：用于癌症成像和治疗的新型蛋白。
The σ2 receptor: a novel protein for the imaging and treatment of cancer.
机构信息
Mallinckrodt Institute of Radiology and ‡Department of Surgery, Washington University School of Medicine , St. Louis, Missouri 63110, United States.
出版信息
J Med Chem. 2013 Sep 26;56(18):7137-60. doi: 10.1021/jm301545c. Epub 2013 Jun 18.
Abstract
The σ2 receptor is an important target for the development of molecular probes in oncology because of its 10-fold higher density in proliferating tumor cells compared with that in quiescent tumor cells and because of the observation that σ2 receptor agonists are able to kill tumor cells via apoptotic and nonapoptotic mechanisms. Although recent evidence indicates that the σ2 receptor binding site is localized within the progesterone receptor membrane component 1 (PGRMC1), most information regarding this protein has been obtained using either radiolabeled or fluorescent receptor-based probes and from biochemical analysis of the effect of σ2 selective ligands on cells grown in culture. This article reviews the development of σ2 receptor ligands and presents an overview of how they have been used in vitro and in vivo to increase our understanding of the role of the σ2 receptor in cancer and proliferation.
摘要
σ2 受体是肿瘤学中开发分子探针的重要靶点，因为与静止肿瘤细胞相比，增殖肿瘤细胞中 σ2 受体的密度高 10 倍，并且观察到 σ2 受体激动剂能够通过凋亡和非凋亡机制杀死肿瘤细胞。尽管最近的证据表明 σ2 受体结合位点位于孕激素受体膜成分 1（PGRMC1）内，但关于该蛋白的大多数信息都是使用放射性标记或荧光受体探针以及从细胞培养中 σ2 选择性配体对细胞的生化分析中获得的。本文综述了 σ2 受体配体的发展，并概述了它们在体外和体内的应用，以增加我们对 σ2 受体在癌症和增殖中的作用的理解。
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